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Synthesis and analysis of polyethylene glycol linked P-glycoprotein-specific homodimers based on (−)-stipiamide

✍ Scribed by Merritt B Andrus; Timothy M Turner; Emily P Updegraff; Zuben E Sauna; Suresh V Ambudkar

Publisher
Elsevier Science
Year
2001
Tongue
French
Weight
77 KB
Volume
42
Category
Article
ISSN
0040-4039

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✦ Synopsis

A series of five homodimeric polyethylene glycol (PEG) linked homodimers based on the multidrug resistance reversal agent (-)-stipiamide were made and tested for their ability to interact with P-glycoprotein, the protein responsible for multidrug resistance, using ATPase and photoaffinity displacement assays. Key reactions include a new alkoxide-mesylate displacement for the assembly of the PEG linkers and a double Sonogashira coupling reaction.

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